In vitro and mouse studies identified small molecule PLK4
inhibitors that could help treat breast cancer. Computational modeling,
chemical synthesis and in vitro testing of (indazolyl)methylene
indolinone analogs identified several lead compounds as selective, nanomolar
inhibitors of PLK4. In multiple human breast cancer cell lines, one lead
compound inhibited growth at low nanomolar IC50 values. In mice
with xenograft breast tumors, the lead compound decreased tumor growth
compared with vehicle. Ongoing work includes IND-enabling studies of an
optimized PLK4 inhibitor and planning of a Phase I trial of that inhibitor to
treat solid tumors.

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